Document Report Card
Basic Information
ID: ALA1933064
Journal: Bioorg Med Chem Lett
Title: Synthesis and evaluation of potential inhibitors of human and Escherichia coli histidine triad nucleotide binding proteins.
Authors: Bardaweel SK, Ghosh B, Wagner CR.
Abstract: Based on recent substrate specificity studies, a series of ribonucleotide based esters and carbamates were synthesized and screened as inhibitors of the phosphoramidases and acyl-AMP hydrolases, Escherichia coli Histidine Triad Nucleotide Binding Protein (ecHinT) and human Histidine Triad Nucleotide Binding Protein 1 (hHint1). Using our established phosphoramidase assay, K(i) values were determined. All compounds exhibited non-competitive inhibition profiles. The carbamate based inhibitors were shown to successfully suppress the Hint1-associated phenotype in E. coli, suggesting that they are permeable intracellular inhibitors of ecHinT.
CiteXplore: 22104145